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Comprehensive Target Engagement by the EZH2 Inhibitor Tulmimetostat Allows for Targeting of ARID1A Mutant Cancers.
Keller PJ, Adams EJ, Wu R, Côté A, Arora S, Cantone N, Meyer R, Mertz JA, Gehling V, Cui J, Stuckey JI, Khanna A, Zhao F, Chen Z, Yu Z, Cummings RT, Taimi M, Lakhani NJ, Rasco D, Gutierrez M, Duska L, Devitt M, Rippley R, Levell J, Truong J, Wang J, Sun K, Trojer P. Keller PJ, et al. Among authors: cantone n. Cancer Res. 2024 Aug 1;84(15):2501-2517. doi: 10.1158/0008-5472.CAN-24-0398. Cancer Res. 2024. PMID: 38833522 Free PMC article. Clinical Trial.
GNE-064: A Potent, Selective, and Orally Bioavailable Chemical Probe for the Bromodomains of SMARCA2 and SMARCA4 and the Fifth Bromodomain of PBRM1.
Taylor AM, Bailey C, Belmont LD, Campbell R, Cantone N, Côté A, Crawford TD, Cummings R, DeMent K, Duplessis M, Flynn M, Good AC, Huang HR, Joshi S, Leblanc Y, Murray J, Nasveschuk CG, Neiss A, Poy F, Romero FA, Sandy P, Tang Y, Tsui V, Zawadzke L, Sims RJ 3rd, Audia JE, Bellon SF, Magnuson SR, Albrecht BK, Cochran AG. Taylor AM, et al. Among authors: cantone n. J Med Chem. 2022 Aug 25;65(16):11177-11186. doi: 10.1021/acs.jmedchem.2c00662. Epub 2022 Aug 5. J Med Chem. 2022. PMID: 35930799
Identification and characterization of second-generation EZH2 inhibitors with extended residence times and improved biological activity.
Stuckey JI, Cantone NR, Côté A, Arora S, Vivat V, Ramakrishnan A, Mertz JA, Khanna A, Brenneman J, Gehling VS, Moine L, Sims RJ 3rd, Audia JE, Trojer P, Levell JR, Cummings RT. Stuckey JI, et al. Among authors: cantone nr. J Biol Chem. 2021 Jan-Jun;296:100349. doi: 10.1016/j.jbc.2021.100349. Epub 2021 Jan 30. J Biol Chem. 2021. PMID: 33524394 Free PMC article.
Discovery of CPI-1612: A Potent, Selective, and Orally Bioavailable EP300/CBP Histone Acetyltransferase Inhibitor.
Wilson JE, Patel G, Patel C, Brucelle F, Huhn A, Gardberg AS, Poy F, Cantone N, Bommi-Reddy A, Sims RJ 3rd, Cummings RT, Levell JR. Wilson JE, et al. Among authors: cantone n. ACS Med Chem Lett. 2020 Apr 23;11(6):1324-1329. doi: 10.1021/acsmedchemlett.0c00155. eCollection 2020 Jun 11. ACS Med Chem Lett. 2020. PMID: 32551019 Free PMC article.
Design, Synthesis, and Pharmacological Evaluation of Second Generation EZH2 Inhibitors with Long Residence Time.
Khanna A, Côté A, Arora S, Moine L, Gehling VS, Brenneman J, Cantone N, Stuckey JI, Apte S, Ramakrishnan A, Bruderek K, Bradley WD, Audia JE, Cummings RT, Sims RJ 3rd, Trojer P, Levell JR. Khanna A, et al. Among authors: cantone n. ACS Med Chem Lett. 2020 Mar 26;11(6):1205-1212. doi: 10.1021/acsmedchemlett.0c00045. eCollection 2020 Jun 11. ACS Med Chem Lett. 2020. PMID: 32551002 Free PMC article.
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